1. Field of the Invention
The present invention relates to novel topical base compositions having a unique combination of ingredients, and weight percents thereof, for use as effective carrier vehicles for one or a plurality of active agents that are to be applied topically to the skin of a human being or animal, such as hydrocortisone, in active agent-containing compositions.
The present invention also relates to novel active agent-containing compositions, such as those that include hydrocortisone (alone or in a combination with one or more other active ingredients), or one or more other active agents, such as skin lightening or whitening agents, for a topical application to the skin of a human being or animal having a unique combination of ingredients, and weight percents thereof, which have been determined to have many advantages in comparison with other topical active-agent containing compositions. For example, they penetrate one or more layers of, and tissues in, the skin, and have been determined to be extremely efficacious in promoting a repair, an improvement or a complete healing of a wide variety of different skin disorders, diseases and/or conditions, including inflammation (acting as an anti-inflammatory agent), deep within the layers and tissues of the skin, including the epidermis and dermis.
The present invention further relates to methods for producing the above formulations, and methods for improving, repairing, healing, lightening or whitening, or otherwise treating the skin of a mammal with respect to a wide variety of different disorders, diseases and/or conditions, such as those that are described herein, and/or causing the mammal's skin to feel soothed, softened and/or conditioned, by topically administering, or otherwise applying, effective amounts of the composition thereto.
2. Background
The skin of mammals, such as human beings and animals of all ages, and animals of all types, often becomes diseased, traumatized, inflamed, reddened, injured, irritated, damaged, deteriorated, cracked, itchy, severely dried, covered with a plurality of bumps and/or blisters, acne and/or insect bites, or otherwise wounded as a result of a wide variety of causes. These causes include, but are not limited to, physical injury, trauma, perforation, cutting, burning (by sun exposure, flame, hot objects and/or the like), blistering (from sun exposure, other burning, shoes and/or the like), chapping, bites (by insects, animals, human beings and/or the like), disease or disorder (poison ivy, poison oak, genital disease and/or the like), illness, microbes, exposure to chemicals, exposure to harsh environmental conditions (extreme hot or cold conditions, high winds, or the like), age, abuse, extreme dryness, and/or other factors.
In order to improve or promote a healing of the above (and other) types of skin problems in both human beings and animals, it is often necessary, or at least desirable, to employ one or more topical compositions for a topical application to the skin that include one or more active agents in a base having an ability to act as a carrier vehicle for the active agents when topically applied to the skin, such as a hydrocortisone-containing ointment or cream for topical application to the skin. However, very disadvantageously, many of the known topical skin compositions that contain hydrocortisone and/or other active agents do not penetrate the skin, or various layers thereof, or tissues present therein, but in contrast, are only designed to lay on top of the skin stratum corneum (the outermost layer of the epidermis, or external skin surface). As a result, these topical compositions often are not very efficacious, or at all efficacious, in repairing, improving or healing one or more skin disorders, diseases or adverse conditions, such as an inflammation or redness that extends deep within the various layers of, and tissues present in, the skin.
Moreover, very disadvantageously, many of the base formulations that are presently employed as carrier vehicles for topically applied active agents are very greasy and messy, often soiling the clothing of the user, are not convenient for use by consumers and/or are subject to deterioration under one or more adverse environmental conditions (i.e., they deteriorate), such as high temperatures. For example, the base formulations that are employed in some of the known and commercially-available rigid stick formulations for a topical application to the skin and/or lips crack in relatively cold temperatures and/or melt in relatively high temperatures, causing the product to become less useful or completely useless, and often extremely messy and a waste of money. Because many of these products include high quantities of “oily” and/or “fatty” types of substances, if such substances melt under conditions of relatively high heat, such as when they are left in a glove box of a vehicle during hot summer months, the oils and/or fats, which generally are not soluble in water or in aqueous-based cleaning agents, can be extremely difficult to remove from papers, clothing and similar types of items, upon which they may melt and/or spill when melted.
Moreover, most existing topical skin compositions have either a very thick feel, lacking cosmetic elegance and therefore decreasing compliance, or a thin feel, which may increase compliance, but decreases efficacy greatly because an ability to decrease transepidermal water loss (TEWL) is very important for any of these medications, and is often lacking therefrom.
There are very few, if any, topical skin medications including hydrocortisone (and/or other active ingredients) on the market that are present in a solid form, such as a stick, allowing a user to treat an area of skin disease that is very small, such as a size of a pinpoint, or very large, such as a plurality of square inches in diameter, and effectively seal the skin off from further damage, all the while decreasing transepidermal water loss (TEWL) and repairing or fully healing the skin. Additionally, those topical skin medications that include hydrocortisone usually have an undesirable “tacky” feel to them, and have a very bitter taste and odor if applied to the mucosal areas of the lips, which is also very undesirable, and renders their efficacy less likely due to poor patient compliance. To date, none of the existing hydrocortisone balm lip formulations appear to have solved this problem of having a bitter taste. Additionally, none of these formulations have a relatively solid consistency, leaving them unlikely to repair, improve or heal the skin of a patient for long periods of time, as they come off of the skin easily.
Furthermore, none of the topical skin preparations including hydrocortisone in a stick formulation that are on the market have the directive of having one or two types of methods and/or sizes to apply to either large or small surfaces of the skin. For this reason, they are severely limited when it comes to the uses and applicability over various body surface areas. For example, if one likens this to another process, if one only had one size of a paint brush that was no larger than a toothbrush in size, the paint brush would limit the uses of this product. Interestingly, while hydrocortisone has been available for many years, and other formulations have attempted to apply it as a cream to the body, or even as an ointment, there have been no commercially-available products that combine a palatable and elegant form of it in a lip-based product as well as in a product that is suitable for larger body surfaces. None of the existing formulations appear to have a large body application methodology, as they only have a ‘lip balm’ size. They are not indicated for the body, and there is no inducement on any packaging or promotional material for the finger or hand cracks that occur in the drier times of the year or with various skin diseases.
Additionally, the topical skin products including hydrocortisone that have been marketed for over-the-counter treatments have typically been very limited as to treatment of significant skin disease, as they have been creams or ointments. These preparations typically have less penetration and less efficacy on adverse skin conditions, such as psoriasis and eczema, and therefore, generally have little or no healing or other effect on the skin of the majority of patients. As a result, none of these existing hydrocortisone products have any indication of usage for skin diseases other than chapped lips generally or chapped lips in patients with psoriasis or who are taking Accutane or Soriatane (i.e., drugs that cause chapped lips), or related efficacy.
In view of the above, it would be extremely beneficial to provide, and treat the skin of mammals having one or a plurality of skin conditions, disorders, diseases and/or the like, with a topical composition for application to the skin including one or more active agents, such as hydrocortisone, that: (i) penetrates one or a plurality of layers of the mammal's skin, including the epidermis and dermis, and the tissues therein, thereby exhibiting efficacious repair, complete healing and/or other beneficial actions in connection with a variety of different skin problems, such as eczema, psoriasis, dermatitis, seborrheic dermatitis or severe dryness, deep within the layers and/or tissues of the skin (rather than only resting on top of the outside of the outermost layer of the mammal's skin); (ii) has an ability to decrease or prevent transepidermal water loss (TEWL) from the skin and effectively partially or fully seal the skin off from further environmental and/or other damage; (iii) does not have an undesirable feel to the touch or skin of a mammal, such as a very thick, very thin or tacky (sticky) feel, but rather has a relatively smooth, non-tacky, non-sticky and desirable feel; (iv) has a pleasant or desirable taste and odor to a user when applied to mucosal areas of the lips (or elsewhere); (v) may be formed into a wide variety of sizes and/or shapes, or in multiple sizes and/or shapes, (vi) may be applied as a product over various different body surface areas of different sizes and/or types, such as a lip-based product for application to the lips and also as separate products that are suitable for topical application to larger body surfaces and, thus, permit a user to treat very small and/or very large areas of the skin (such as a pinpoint area and/or an area spanning one or a plurality of square inches or other shapes); (vii) is convenient and easy to administer for users; (viii) is safe and reliable for use by mammals; (ix) maintains its consistency, form and shape under relatively extreme environmental conditions, such as at relatively low temperatures, for example, on a ski slope, and at relatively high temperatures, for example, in a hot vehicle during the summer months; (x) is cosmetically elegant and physically appealing and desirable; (xi) promotes or otherwise enhances patient compliance; and (xii) is relatively inexpensive.
It would also be extremely beneficial to provide base compositions that have the above characteristics, and can properly function as carrier vehicles for one or more active agents to be applied topically to the skin of a human being or animal.
3. Description of Related Art
According to the Internet web site burl's bees dot com, Burt's Bees lip balm, which is present in a tube, contains beeswax, cocos nucifera (coconut) oil, helianthus annuus (sunflower) seed oil, mentha piperita (peppermint) oil, lanolin, tocopherol, rosmarinus officinalis (rosemary) leaf extract, glycine soja (soybean) oil, canola oil, Tin: cera alba (beeswax, cire d'abeille), cocos nucifera (coconut) oil, prunus amygdalus dulcis (sweet almond) oil, mentha piperita (peppermint) oil, lanolin, tocopherol, rosmarinus officinalis (rosemary) leaf extract, glycine soja (soybean) oil and canola oil (huile de colza).
According to the web site chapstick dot com, ChapStick® contains seven natural ingredients that function as skin-conditioning agents or moisturizers, which remain on the surface of the skin. Some of these ingredients are also stated to prevent evaporation of water and protect lips from drying and chapping when exposed to wind or cold weather. The process of manufacturing ChapStick® is stated to be similar to following a recipe. A big blender is stated to mix the heated ingredients of ChapStick®. The color and flavor are added, and then the warm mixture is poured into containers.
Carmex is a brand of topical lip balm that is meant to improve or eliminate cold sores and soothe dry or chapped lips. It may be sold in jars, sticks and squeezable tubes. According to the Internet web site mycarmex dot com, traditional Carmex contains camphor, menthol, phenol, beeswax, cetyl esters, flavor, fragrance, lanolin, paraffin, petrolatum, salicylic acid and theobroma cacao(cocoa) seed butter.
According to the Internet web site blistex dot com, Blistex medicated lip balm (in the form of a hard stick), contains the active ingredients dimethicone (2.0%) (skin protectant), oxybenzone (2.5%) (sunscreen) and padimate 0 (6.6%) (sunscreen), as well as the other ingredients bees wax, camphor, cetyl alcohol, cetyl Palmitate, euphorbia cerifera (candelilla) wax, flavors, isopropyl Myristate, isopropyl Palmitate, isopropyl stearate, lanolin, lanolin oil, menthol, methylparaben, mineral oil, ozokerite, paraffin, petrolatum, polybutene, propylparaben, red 6 lake, theobroma cacao (cocoa) seed butter and titanium dioxide.
U.S. Pat. No. 5,662,993 describes stick formulations for topical delivery of water soluble and/or water insoluble agents, which may contain steroids, antibiotics, antifungals, antihistamines, anti-inflammatories or local anesthetics. The vehicles comprise a combination of waxes and oils and a surfactant in embodiments involving water soluble agents.
U.S. Pat. No. 6,228,351 describes a lip balm for treating cheilitis (painful dry inflamed lips) containing from 0.2% to 2.5% hydrocortisone in a base of beeswax mineral oil and petroleum jelly, wherein the amount of petroleum jelly is not more than that of the beeswax and mineral oil combined, and the amount of mineral oil is roughly equal to the amount of beeswax. In contrast with the compositions and base formulations of the present invention, the lip balms described by the '351 patent, which contain many different ingredients, and weight percents thereof, such as large quantities of petroleum jelly (from 40% to 50% by weight of the base), are used only upon the lips, and disadvantageously have an undesirable taste, which is typical of hydrocortisone-containing products (and tends to discourage, reduce or eliminate patient compliance). Further, as a result of its different ingredients, particularly the large amount of petroleum jelly, these lip balms have a very different consistency in comparison with the hydrocortisone-containing (and other) compositions of the present invention. They have a liquid or semi-liquid type of a feel to the touch (i.e., not a solid feel), and may be messy and/or sloppy for use by individuals, and to their clothing, jewelry and surrounding objects (papers, books, maps, sunglasses, seat or car and/or the like), particularly when present at high temperatures. Further, these lip balms are not indicated by the '351 patent for any skin malady or condition other than psoriasis, and have not been shown by the '351 patent to be efficacious for any such malady or condition.
Published U.S. Patent Application No. US 2004/0091539 A1 describes a solid stick topical composition containing a corticosteroid, petrolatum, wax, propyleneglycol and an emulsifier.
Published U.S. Patent Application No. US 2003/0232091 A1 describes a controlled release system for stabilizing retinol, retinol derivatives, and extracts containing retinol in cosmetic, dermatological, and pharmaceutical compositions.
Published U.S. Patent Application No. US 2004/0202725 A1 describes compositions for the treatment of pilosebaceous gland inflammations, especially of the hair follicle and its appendages, in particular of Acne Vulgaris and Folliculitis, comprising as active ingredient aluminum fluoride, or chemical compounds that finally release aluminum fluoride.
None of the patent documents or web sites that are identified above describe or suggest the unique base and active agent-containing formulations of the present invention, or the related production or application methods, or compositions having the advantages that are described herein.